5 years ago

Highly Oxidized Guaianolide Sesquiterpenoids with Potential Anti-inflammatory Activity from Chrysanthemum indicum

Highly Oxidized Guaianolide Sesquiterpenoids with Potential Anti-inflammatory Activity from Chrysanthemum indicum
Yu-Cheng Gu, Xiao-Bing Wang, Ling-Yi Kong, Chen Chen, Kang Chen, Gui-Min Xue, Xiao-Qing Li, Jian-Guang Luo
Ten new highly oxidized monomeric (18) and dimeric guaianolides (9 and 10), along with two known guaianolide derivatives (11 and 12), were isolated from the aerial parts of Chrysanthemum indicum using a bioassay-guided fractionation procedure. The new compounds were characterized by the basic analysis of the spectroscopic data obtained, and the absolute configurations were determined by both empirical approaches and ECD calculations. Inhibitory effects of 112 on nitric oxide production were investigated in lipopolysaccaride (LPS)-mediated RAW 264.7 cells, and most of them (18 and 11) displayed IC50 values in the range 1.4–9.7 μM. Moreover, a mechanistic study revealed that the potential anti-inflammatory activity of compound 1 appears to be mediated via suppression of an LPS-induced NF-κB pathway and down-regulation of MAPK activation.

Publisher URL: http://dx.doi.org/10.1021/acs.jnatprod.7b00867

DOI: 10.1021/acs.jnatprod.7b00867

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